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Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases

Journal of medicinal chemistry, 2020-08, Vol.63 (15), p.7957-7985

2020

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Heterobifunctional Molecules Induce Dephosphorylation of Kinases–A Proof of Concept Study

Journal of medicinal chemistry, 2020-03, Vol.63 (6), p.2807-2813

2020

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Monomeric Targeted Protein Degraders

Journal of medicinal chemistry, 2020-10, Vol.63 (20), p.11330-11361

2020

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Overcoming Preclinical Safety Obstacles to Discover (S)‑N‑((1,2,3,5,6,7-Hexahydro‑s‑indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro‑5H‑pyrazolo[5,1‑b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor

Journal of medicinal chemistry, 2022-11, Vol.65 (21), p.14721-14739

2022

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Selective activation of PFKL suppresses the phagocytic oxidative burst

Cell, 2021-08, Vol.184 (17), p.4480-4494.e15

2021

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Identifying transcriptional programs underlying cancer drug response with TraCe-seq

Nature biotechnology, 2022-01, Vol.40 (1), p.86-93

2022

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Targeted degradation via direct 26S proteasome recruitment

Nature chemical biology, 2023-01, Vol.19 (1), p.55

2023

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RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy

Cancer discovery, 2022-01, Vol.12 (1), p.204-219

2022

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Discovery of 2‑{3-[2-(1-Isopropyl-3-methyl‑1H‑1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl]‑1H‑pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β‑Sparing Phosphoinositide 3‑Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity

Journal of medicinal chemistry, 2013-06, Vol.56 (11), p.4597-4610

2013

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Correction: MCC950/CRID3 potently targets the NACHT domain of wild-type NLRP3 but not disease-associated mutants for inflammasome inhibition

PLoS biology, 2019-10, Vol.17 (10), p.e3000529-e3000529

2019

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Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability

Journal of medicinal chemistry, 2019-08, Vol.62 (15), p.7032-7041

2019

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Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors

Journal of medicinal chemistry, 2022-09, Vol.65 (17), p.11500-11512

2022

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Ternary complex dissociation kinetics contribute to mutant-selective EGFR degradation

Cell chemical biology, 2023-02, Vol.30 (2), p.175-187.e15

2023

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The Rational Design of Selective Benzoxazepin Inhibitors of the α‑Isoform of Phosphoinositide 3‑Kinase Culminating in the Identification of (S)‑2-((2-(1-Isopropyl‑1H‑1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326)

Journal of medicinal chemistry, 2016-02, Vol.59 (3), p.985-1002

2016

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A Multifaceted Hit-Finding Approach Reveals Novel LC3 Family Ligands

Biochemistry (Easton), 2023-02, Vol.62 (3), p.633-644

2023

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The Crystal Structure of the Catalytic Domain of the NF-κB Inducing Kinase Reveals a Narrow but Flexible Active Site

Structure (London), 2012-10, Vol.20 (10), p.1704-1714

2012

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Back Pocket Flexibility Provides Group II p21-Activated Kinase (PAK) Selectivity for Type I 1/2 Kinase Inhibitors

Journal of medicinal chemistry, 2014-02, Vol.57 (3), p.1033-1045

2014

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Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform

Journal of medicinal chemistry, 2011-11, Vol.54 (22), p.7815-7833

2011

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Structure Based Design of Potent Selective Inhibitors of Protein Kinase D1 (PKD1)

ACS medicinal chemistry letters, 2019-09, Vol.10 (9), p.1260-1265

2019

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Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles

ACS medicinal chemistry letters, 2017-09, Vol.8 (9), p.936-940

2017

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Abstract DDT02-01: Discovery of GDC-0077, a highly isoform selective inhibitor of PI3Kα that promotes selective loss of mutant-p110α

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.DDT02-01-DDT02-01

Staben, Steven T.

2017

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Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties

Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases

Heterobifunctional Molecules Induce Dephosphorylation of Kinases–A Proof of Concept Study

Monomeric Targeted Protein Degraders

Overcoming Preclinical Safety Obstacles to Discover (S)‑N‑((1,2,3,5,6,7-Hexahydro‑s‑indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro‑5H‑pyrazolo[5,1‑b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor

Selective activation of PFKL suppresses the phagocytic oxidative burst

NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus

Identifying transcriptional programs underlying cancer drug response with TraCe-seq

Targeted degradation via direct 26S proteasome recruitment

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα

RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy

Discovery of 2‑{3-[2-(1-Isopropyl-3-methyl‑1H‑1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl]‑1H‑pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β‑Sparing Phosphoinositide 3‑Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity

Correction: MCC950/CRID3 potently targets the NACHT domain of wild-type NLRP3 but not disease-associated mutants for inflammasome inhibition

Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability

Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors

Ternary complex dissociation kinetics contribute to mutant-selective EGFR degradation

The Rational Design of Selective Benzoxazepin Inhibitors of the α‑Isoform of Phosphoinositide 3‑Kinase Culminating in the Identification of (S)‑2-((2-(1-Isopropyl‑1H‑1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326)

A Multifaceted Hit-Finding Approach Reveals Novel LC3 Family Ligands

The Crystal Structure of the Catalytic Domain of the NF-κB Inducing Kinase Reveals a Narrow but Flexible Active Site

Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K)

Back Pocket Flexibility Provides Group II p21-Activated Kinase (PAK) Selectivity for Type I 1/2 Kinase Inhibitors

Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform

Structure Based Design of Potent Selective Inhibitors of Protein Kinase D1 (PKD1)

Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles

Abstract DDT02-01: Discovery of GDC-0077, a highly isoform selective inhibitor of PI3Kα that promotes selective loss of mutant-p110α

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